Marco Peters
Scripps Health
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Publication
Featured researches published by Marco Peters.
Journal of Medicinal Chemistry | 2017
Laurent Gomez; Mark Eben Massari; Troy Vickers; Graeme Freestone; William F. Vernier; Kiev S. Ly; Rui Xu; Margaret A. McCarrick; Tami Marrone; Markus Metz; Yingzhou G. Yan; Zachary W. Yoder; Robert H. Lemus; Nicola J. Broadbent; Richard Barido; Noelle Warren; Kara R. Schmelzer; David Neul; Dong Lee; Carsten B. Andersen; Kristen Sebring; Kathleen Aertgeerts; Xianbo Zhou; Ali Tabatabaei; Marco Peters; J. Guy Breitenbucher
A series of potent and selective [1,2,4]triazolo[1,5-a]pyrimidine PDE2a inhibitors is reported. The design and improvement of the binding properties of this series was achieved using X-ray crystal structures in conjunction with careful analysis of electronic and structural requirements for the PDE2a enzyme. One of the lead compounds, compound 27 (DNS-8254), was identified as a potent and highly selective PDE2a enzyme inhibitor with favorable rat pharmacokinetic properties. Interestingly, the increased potency of compound 27 was facilitated by the formation of a halogen bond with the oxygen of Tyr827 present in the PDE2a active site. In vivo, compound 27 demonstrated significant memory enhancing effects in a rat model of novel object recognition. Taken together, these data suggest that compound 27 may be a useful tool to explore the pharmacology of selective PDE2a inhibition.
Journal of Medicinal Chemistry | 2018
Vincent J. Santora; Theresa A. Almos; Richard Barido; Jillian Basinger; Chris L. Bellows; Brett C. Bookser; J. Guy Breitenbucher; Nicola J. Broadbent; Clifford Cabebe; Chih-Kun Chai; Mi Chen; Stephine Chow; De Michael Chung; Lindsay Crickard; Anne Danks; Graeme Freestone; Dany Gitnick; Varsha Gupta; Christine Hoffmaster; Andrew Richard Hudson; Alan P. Kaplan; Michael R. Kennedy; Dong Lee; James Limberis; Kiev Ly; Chi Ching Mak; Brittany Masatsugu; Andrew Morse; Jim Na; David Neul
We report here the identification and optimization of a novel series of potent GlyT1 inhibitors. A ligand design campaign that utilized known GlyT1 inhibitors as starting points led to the identification of a novel series of pyrrolo[3,4- c]pyrazoles amides (21-50) with good in vitro potency. Subsequent optimization of physicochemical and in vitro ADME properties produced several compounds with promising pharmacokinetic profiles. In vivo inhibition of GlyT1 was demonstrated for select compounds within this series by measuring the elevation of glycine in the cerebrospinal fluid (CSF) of rats after a single oral dose of 10 mg/kg. Ultimately, an optimized lead, compound 46, demonstrated in vivo efficacy in a rat novel object recognition (NOR) assay after oral dosing at 0.1, 1, and 3 mg/kg.
Journal of Medicinal Chemistry | 2017
Brian Dyck; Bryan Branstetter; Tawfik Gharbaoui; Andrew Richard Hudson; J. Guy Breitenbucher; Laurent Gomez; Iriny Botrous; Tami Marrone; Richard Barido; Charles K. Allerston; E. Peder Cedervall; Rui Xu; Vandana Sridhar; Ryan Barker; Kathleen Aertgeerts; Kara Schmelzer; David Neul; Dong Lee; Mark Eben Massari; Carsten B. Andersen; Kristen Sebring; Xianbo Zhou; Robert Petroski; James Limberis; Martin Augustin; Lawrence E. Chun; Thomas E. Edwards; Marco Peters; Ali Tabatabaei
Current opinion in behavioral sciences | 2015
Marco Peters; Mónica Muñoz-López; Richard G. M. Morris
Archive | 2013
Amy Allan; Bryan Branstetter; Brian Dyck; Michael I. Weinhouse; Laurent Gomez; Tammi Jo Marrone; Marco Peters
Archive | 2013
Bryan Branstetter; James Guy Breitenbucher; Brian Dyck; Laurent Gomez; Andrew Richard Hudson; Tami Marrone; Marco Peters; Troy Vickers; Michael I. Weinhouse
Archive | 2017
Amy Allan; Brian Dyck; Bryan Branstetter; Laurent Gomez; Marco Peters; Michael I. Weinhouse; Tammi Jo Marrone
Archive | 2017
Amy Allan; Bryan Branstetter; Brian Dyck; Michael I. Weinhouse; Laurent Gomez; Tami Marrone; Marco Peters
Archive | 2017
Andrew Richard Hudson; Brian Dyck; Bryan Branstetter; James Guy Breitenbucher; Laurent Gomez; Marco Peters; Tami Marrone; Troy Vickers
Archive | 2017
Brian Dyck; Marco Peters; J. Guy Breitenbucher